PF-4989216
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406267

CAS#: 1276553-09-3

Description: PF-4989216 is a novel potent and selective PI3K inhibitor. PF-4989216 inhibits the phosphorylation of PI3K downstream molecules and subsequently leads to inhibition in cell proliferation and xenograft tumor growth in NSCLCs harboring a PIK3CA mutation, including an erlotinib resistant line, NCI-H1975. PF-4989216 inhibited PI3K downstream signaling and subsequently led to apoptosis induction, and inhibition in cell viability, transformation, and xenograft tumor growth in SCLCs harboring PIK3CA mutation.

Chemical Structure

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PF-4989216
CAS# 1276553-09-3
Instruction

Theoretical Analysis

MedKoo Cat#: 406267
Name: PF-4989216
CAS#: 1276553-09-3
Chemical Formula: C18H13FN6OS
Exact Mass: 380.09
Molecular Weight: 380.399
Elemental Analysis: C, 56.83; H, 3.44; F, 4.99; N, 22.09; O, 4.21; S, 8.43

Price and Availability

Size Price Availability Quantity
5mg USD 250 2 Weeks
10mg USD 450 2 Weeks
50mg USD 1050 2 Weeks
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Synonym: PF4989216; PF 4989216; PF-4989216.

IUPAC/Chemical Name: 4-(4-cyano-2-fluorophenyl)-2-morpholino-5-(1H-1,2,4-triazol-5-yl)thiophene-3-carbonitrile

InChi Key: MUENOTXSRZEFJV-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H13FN6OS/c19-14-7-11(8-20)1-2-12(14)15-13(9-21)18(25-3-5-26-6-4-25)27-16(15)17-22-10-23-24-17/h1-2,7,10H,3-6H2,(H,22,23,24)

SMILES Code: N#CC1=C(N2CCOCC2)SC(C3=NC=NN3)=C1C4=CC=C(C#N)C=C4F

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: soluble in DMSO

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:         

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 380.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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 1: Walls M, Baxi SM, Mehta PP, Liu KK, Zhu J, Estrella H, Li C, Zientek M, Zong
Q, Smeal T, Yin MJ. Targeting small cell lung cancer harboring PIK3CA mutation
with a selective oral PI3K inhibitor PF-4989216. Clin Cancer Res. 2014 Feb
1;20(3):631-43. doi: 10.1158/1078-0432.CCR-13-1663. Epub 2013 Nov 15. PubMed
PMID: 24240111.